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  • Title: (11)C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand.
    Author: Andersen VL, Hansen HD, Herth MM, Dyssegaard A, Knudsen GM, Kristensen JL.
    Journal: Bioorg Med Chem Lett; 2015 Mar 01; 25(5):1053-6. PubMed ID: 25655720.
    Abstract:
    Pimavanserin is a selective serotonin 2A receptor (5-HT2AR) inverse agonist that has shown promise for treatment of psychotic symptoms in patients with Parkinson's disease. Here, we detail the (11)C-labeling and subsequently evaluate pimavanserin as a PET-radioligand in pigs. [(11)C]Pimavanserin was obtained by N-methylation of an appropriate precursor using [(11)C]MeOTf in acetone at 60°C giving radiochemical yields in the range of 1-1.7GBq (n=4). In Danish Landrace pigs the radio ligand readily entered the brain and displayed binding in the cortex in accordance with the distribution of 5-HT2ARs. However, this binding could not be blocked by either ketanserin or pimavanserin itself, indicating high nonspecific binding. The lack of displacement by the 5-HT2R antagonist and binding in the thalamus suggests that [(11)C]pimavanserin is not selective for the 5-HT2AR in pigs.
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